反応式
Cl[C:2]1[N:7]=[C:6]([C:8]2[C:9]([C:18]3[CH:19]=[C:20]([NH:24][C:25](=[O:32])[CH2:26][C:27]4[S:28][CH:29]=[CH:30][CH:31]=4)[CH:21]=[CH:22][CH:23]=3)=[N:10][N:11]3[CH:16]=[C:15]([CH3:17])[CH:14]=[CH:13][C:12]=23)[CH:5]=[CH:4][N:3]=1.[N:33]1([CH2:38][C:39]2[CH:40]=[C:41]([NH2:45])[CH:42]=[CH:43][CH:44]=2)[CH2:37][CH2:36][CH2:35][CH2:34]1.Cl>O1CCOCC1.CC(O)C>[CH3:17][C:15]1[CH:14]=[CH:13][C:12]2[N:11]([N:10]=[C:9]([C:18]3[CH:19]=[C:20]([NH:24][C:25](=[O:32])[CH2:26][C:27]4[S:28][CH:29]=[CH:30][CH:31]=4)[CH:21]=[CH:22][CH:23]=3)[C:8]=2[C:6]2[CH:5]=[CH:4][N:3]=[C:2]([NH:45][C:41]3[CH:42]=[CH:43][CH:44]=[C:39]([CH2:38][N:33]4[CH2:34][CH2:35][CH2:36][CH2:37]4)[CH:40]=3)[N:7]=2)[CH:16]=1参加物
6
実験手順
N-{3-[3-(2-chloro-4-pyrimidinyl)-6-methylpyrazolo[1,5-a]pyridin-2-yl]phenyl}-2-(2-thienyl)acetamide (100 mg, 0.22 mml), [3-(1-pyrrolidinylmethyl)phenyl]amine (46 mg, 0.26 mmol), and 4N HCl in dioxane (0.10 mL) were combined in i-PrOH (3 mL) in a procedure analogous to Example 67, Step B to afford the title compound as a yellow solid (70 mg, 53%). 1H NMR (300 MHz, DMSO-d6) δ 10.40 (s, 1H), 9.55 (s, 1H), 8.71 (s, 1H), 8.47 (d, J=9.8 Hz, 1H), 8.26 (d, J=5.3 Hz, 1H), 7.91 (s, 1H), 7.78 (d, J=7.7 Hz, 1H), 7.72-7.67 (m, 2H), 7.48-7.36 (m, 3H), 7.31-7.19 (m, 2H), 7.00-7.01 (m, 2H), 6.92 (d, J=7.5 Hz, 1H), 6.50 (d, J=5.6 Hz, 1H), 3.91 (s, 2H), 3.57 (s, 2H), 2.52-2.45 (m, 4H), 2.41 (s, 3H), 1.74-1.69 (m, 4H). ES-LC/MS m/z=600 [M+H]+.
出典と根拠
- ORDレコード
- ord-0c19a51f30d64128937ec9c7a4e6c473
- 出典データセット
- uspto-grants-2010_10
- 特許番号
- US07807673B2
関連ノート
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